Assay Detail
Binding
CHEMBL3399462
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human GAT1 expressed in HEK293 cells using NO71156 as unlabelled marker by LC-ESI-MS-MS based competitive MS binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL1903) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.99 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 7.32 |
| CHEMBL3398501 | — | — | 1 | 7.18 |
| CHEMBL3398499 | — | — | 1 | 6.67 |
| CHEMBL3398500 | — | — | 1 | 5.96 |
| CHEMBL3398498 | — | — | 1 | 5.40 |
| CHEMBL3398507 | — | — | 1 | 4.72 |
| CHEMBL3398506 | — | — | 1 | 4.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | Ki | = | 47.86 | nM | 7.32 |
| CHEMBL3398501 | — | Ki | = | 66.07 | nM | 7.18 |
| CHEMBL3398499 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL3398500 | — | Ki | = | 1096.48 | nM | 5.96 |
| CHEMBL3398498 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL3398507 | — | Ki | = | 19054.61 | nM | 4.72 |
| CHEMBL3398506 | — | Ki | = | 20417.38 | nM | 4.69 |